| 货号 | 18427-10mg |
| 描述 | Fluphenazine is a traditional antipsychotic compound that tightly binds the dopamine D2 receptor (Ki = 0.55 nM) and also reversibly inhibits calmodulin at micromolar concentrations.1,2 Fluphenazine-N-2-chloroethane is a derivative of fluphenazine that contains an alkylating chlorethylamine chain, which produces irreversible protein binding.3,4 It is a relatively selective, irreversible antagonist of D2 receptors both in vitro(IC50 = 100 nM) and in vivo, inactivating approximately 90% of D2 receptors in mice within 4 hours of treatment.5,6 Through this action, fluphenazine-B-2-chloroethane can be used to induce catalepsy in mice.5,7 It irreversibly inhibits calmodulin at higher doses (IC50 = 10 µM), which can sensitize cancer cells to TRAIL-induced apoptosis.3,8 |
| 别名 | Fluphenazine-N-mustard;FNM;FPCE;SKF-7171A; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Seeman, P. Atypical antipsychotics: Mechanism of action. Can.J.Psychiatry 47(1), 27-38 (2002). 2.OCallaghan, J.P.,Dunn, L.A., and Lovenberg, W. Calcium-regulated phosphorylation in synaptosomal cytosol: Dependence on calmodulin. Proceedings of the National Academy of Sciences of the United States of America 77(10), 5812-5816 (1980). 3.Winkler, J.D.,Thermos, K., and Weiss, B. Differential effects of fluphenazine-N-mustard, on calmodulin activity and on D1 and D2 dopaminergic responses. Psychopharmacology (Berl) 92(3), 285-291 (1987). 4.Hait, W.N.,Glazer, L.,Kaiser, C., et al. Pharmacological properties of fluphenazine-mustard, an irreversible calmodulin antagonist. Molecular Pharmacology 32(3), 404-409 (1987). 5.Qin, Z.H.,Zhou, L.W.,Zhang, S.P., et al. D2 dopamine receptor antisense oligodeoxynucleotide inhibits the synthesis of a functional pool of D2 dopamine receptors. Molecular Pharmacology 48(4), 730-737 (1995). 6.Thermos, K.,Winkler, J.D., and Weiss, B. Comparison of the effects of fluphenazine-N-mustard on dopamine binding sites and on behavior induced by apomorphine in supersensitive mice. Neuropharmacology 26(10), 1473-1480 (1987). 7.Davidkova, G.,Zhou, L.W.,Morabito, M., et al. D2 dopamine antisense RNA expression vector, unlike haloperidol, produces long-term inhibition of D2 dopamine-mediated behaviors without causing up-regulation of D2 dopamine receptors. Journal of Pharmacology and Experimental Therapeutics 285(3), 1187-1196 (1998). 8.Hwang, M.K.,Min, Y.K., and Kim, S.H. Calmodulin inhibition contributes to sensitize TRAIL-induced apoptosis in human lung cancer H1299 cells. Biochemistry and Cell Biology 87(6), 919-926 (2009). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 528.9 |
| 分子式 | C22H25ClF3N3S • 2HCl |
| CAS号 | 3892-78-2 |
| 稳定性 | ≥ 2 years |
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